1. Field
One or more embodiments of the present invention relate to a novel compound, a preparing method thereof, and a use thereof as an inhibitor of histone demethylase.
2. Description of the Related Art
Transcriptional regulation in a cell is a complicated biological procedure. One of the transcriptional regulation mechanisms is post-transcriptional modification of eight histone proteins forming a histone core complex, which are also called histone proteins H2A/B, H3, and H4. N-terminal modification of histone proteins may be, for example, acetylation or methylation of a lysine residue or phosphorylation of a serine residue. Such a medication may change affinity between a histone and a DNA and thereby regulate gene expression.
Methylation of a histone may inhibit or activate transcription. A methyl group is added to a histone by histone lysine methyltransferase (HMT or KMT), while a methyl group bound to a histone is removed by histone lysine demethylase (KDM). KMT is specific to lysine or arginine and may combine one to three methyl groups with a target amino acid residue. KDM is classified as KDM1, KDM2, KDM3, KDM4, KDM5, KDM6, and KDM7 based on the substrate specificity and protein domain structure thereof. An inhibitor of KTM is, for example, chaetocin, DANep, BIX-01294, EGCG, sinefungin, adenoine dialdehyde, and novobiocin. An inhibitor of KDM is, for example, tranylcyprome, phenelzine, a polyamine analogue, N-oxalyglycine (NOG), disulfuram, ebselen, and an N-oxalyl D-tyrosine derivative. These inhibitors are very rare. Therefore, it is necessary to search for an inhibitor which may specifically inhibit KTM or KDM.
A biological approach has come to the fore in natural product research to search for a structurally novel bioactive substance. In recent, studies of bacteria, which are originated from biological backgrounds of insect, have been made actively. In addition, there is need to screen biologically active molecules from bacteria discovered in an environment in which insects grow.
While screening and studying insect-derived microbes, a novel strain producing a novel compound was discovered and KDM activity of the compound was verified to complete the present invention.